selective

Selective PI3Kδ Inhibitor 1 is a PI3Kδ Inhibitor( IC50 = 0.9 nM).

TRPV2-selective blocker 1 (compound IV2-1) is a selective inhibitor of the TRPV2 channel, with an IC50 value of 6.3 μM, specifically targeting the TRPV2 channel without affecting TRPV1, TRPV3, or TRPV4 channels, and effectively suppresses TRPV2-mediated calcium influx in macrophages, inhibiting their phagocytic activity [1].

FKBP51F67V-selective antagonist Ligand2 (example 3-3), a potent ligand, selectively binds to FKBP51 F67V variant without affinity for wild-type FKBP51 or FKBP52 [1], and effectively reverses the anxiogenic phenotype resulting from FKBP51 F67V overexpression in the amygdala.

Ritanserin (R 55667) is a highly effective, relatively selective, long-acting 5-HT2 receptor antagonist (IC50: 0.9 nM), with less activity on Histamine H1, Dopamine D2, Adrenergic α1, and Adrenergic α2 receptors.

PF-06821497 is a selective inhibitor of EZH2 with significant tumor growth inhibition.

Bedoradrine sulfate (MN-221 sulfate) is a super-selective beta2 agonist for the treatment of asthma exacerbations and chronic obstructive pulmonary disease.

VTP50469 is a highly selective and orally active inhibitor of Menin-MLL interaction( Ki: 104 pM) and has potently anti-leukemia activity.

Avosentan (Ro 67-0565) is an effective and selective antagonist of the endothelin receptor (ETA receptor).

Pevonedistat (MLN4924) is a potent and selective NEDD8 activating enzyme (NAE) inhibitor (IC50=4.7 nM) with therapeutic potential for myelodysplastic syndromes (MDS) and antitumor activity.

Pexidartinib (PLX-3397) is a capsule containing a small-molecule receptor tyrosine kinase (RTK) inhibitor targeting KIT, CSF1R, and FLT3, with potential antineoplastic activity.

Bedoradrine free base is a novel, highly selective β2-adrenoceptor agonist for the treatment of asthma and chronic obstructive pulmonary disease (COPD).

eCF506 is a potent and selective inhibitor of SRC (IC50 < 0.5 nM)

Olorofim is a novel selective antifungal compound with inhibitory effect on Aspergillus fumigatus DHODH (IC50: 44 nM) and almost no inhibitory effect on human DHODH (>100 uM).Olorofim has good efficacy against various pathogenic filamentous and dimorphic fungi such as Penicillium spp, Dermatophilus spp and Fusarium spp.

Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.

GW4869 (GW69A) is a selective and non-competitive inhibitor of neutral sphingomyelinase N-SMase (IC50=1 μM). GW4869 also inhibits exosome synthesis/release and is commonly used in exosome-related studies.

MCC950 sodium (CP-456773 sodium) is a potent and selective inhibitor of the inflammatory vesicle NLRP3 (IC50=7.5 nM in BMDMs; IC50=8.1 nM in HMDMs). MCC950 sodium has no effect on other inflammatory vesicles such as AIM2, NLRC4 or NLRP1.

RP-6306 is a potent, selective and orally active PKMYT1 inhibitor (IC50= 14 nM). RP-6306 exhibits a high degree of selectivity for PKMYT1 over other kinases in cellular binding assays. RP-6306 exhibits anticancer effects.

L-161982 is a selective antagonist of EP4 receptor. L-161982 could inhibit PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 could alleviate collagen-induced arthritis in mice.

IMP-1710 is a selective UCH-L1 inhibitor with an IC50 value of 38 nM in a fluorescence polarization assay.

Flovagatran (TGN 255) is an orally active, potent, and selective inhibitor of thrombin and parenteral direct factor II.Flovagatran is used to study venous thromboembolism.

Camonsertib (RP-3500) is a selective, orally active ATR kinase inhibitor (ATRi) with an IC50: 1.00 nM in biochemical assays and exhibits potent antitumour effects. Camonsertib is 30 times more selective for ATR than mTOR (IC50: 120 nM) and is a more active inhibitor of ATM, DNA-PK and PI3Kα kinases. PK and PI3Kα kinases.

MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8 12 65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.

Denifanstat (FASN-IN-2) is a fatty acid synthase (FASN) inhibitor (IC50=0.052 μM, EC50=0.072 μM) with selective and oral activity. Denifanstat has been used in studies of steatohepatitis.

CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.

Syrosingopine has selective depleting effect on brain amines is potentiated by combined treatment with disulfiram or fusaric acid, a dopamine beta-hydroxylase inhibitor.

Relamorelin (RM-131), a selective and potent growth hormone-releasing peptide growth hormone secretagogue receptor (GHSR) agonist, is a potent growth hormone-releasing peptide mimetic with a high affinity for the GHS-1a receptor Relamorelin is a centrally permeable pentapeptide that increases growth hormone levels and accelerates gastric emptying and has potential for studying malignant disease.

AR 231453 is a selective and orally available GPR119 agonist,can stimulate β-cell replication and improve islet graft function.

Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.

SX-682 is a potent, selective and orally bioavailable inhibitor of CXCR1/2 ,has the potential to treat castration-resistant prostate cancer.

SCH772984 is an ERK inhibitor that inhibits ERK1 and ERK2 (IC50=4 1 nM) and is highly selective and ATP-competitive. SCH772984 exhibits antitumor activity against BRAF or RAS mutant cells.

ot-730（QLT 091568） is a new selective beta blocker prodrug that can be used to study eye diseases.

MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.

RSL3 (RSL3 1S) is an inhibitor of GPX4, and inhibits system xc- that blocks GSH synthesis (IC50=100 nM). RSL3 is a VDAC-independent activator of ferroptosis that is selective for tumor cells carrying oncogenic RAS.

Galunisertib (LY2157299) is a TGF-β receptor type I (TGF-βRI) inhibitor (IC50=56 nM) that is selective. Galunisertib has antitumor activity and can be used in combination with PD-1 inhibitors.

T3Inh-1 is an effective and selective inhibitor of ppGalNAc-T3 with an IC50 of 7 µM. T3Inh-1 prevents breast cancer cells. T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects.

CCT245737 (SRA737) is an orally active and selective Chk1 inhibitor (IC50: 1.3 nM); CCT245737 shows much less activity against Chk2 (IC50: 2440 nM).

CCT020312 is a selective activator of EIF2AK3 and PERK. CCT020312 durably inhibits cell proliferation and elicits the phosphorylation of EIF2A.

RBN012759, a potent and selective PARP14 inhibitor, decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants.

Ritlecitinib (PF-06651600) is a potent JAK3-selective inhibitor (IC50: 33.1 nM).

SAFit2 is a highly effective and selective fk506 binding protein 51(FKBP51) inhibitor (Ki: 6 nM). SAFit2 can enhance AKT2-AS160 binding and participate in the downstream response of glucocorticoid release in vivo, and is a candidate compound for the treatment of obesity, chronic pain, depression and anxiety.

Dersimelagon (MT-7117) is an orally active, selective agonist for the melanocortin 1 receptor (MC1R), with EC50 values of 8.16 nM (h), 3.91 nM (cm), 1.14 nM (m), and 0.251 nM (r) in human, cynomolgus monkey, mouse, and rat, respectively. It exhibits strong affinity for human MC1R and MC4R, with Ki values of 2.26 nM and 32.9 nM, respectively. The compound is used in the study of skin pigmentation.

diABZI STING agonist-1 (Tautomerism) (diABZI STING agonist (Compound 3)) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

PLX-4720, a potent and selective inhibitor of B-Raf (V600E) with an IC50 of 13 nM, is equally effective against c-Raf-1 (Y340D and Y341D mutations).

VB124 is an orally active, potent, and selective MCT4 inhibitor, demonstrating specificity in hindering lactate efflux, with IC50 values of 8.6 nM and 19 nM for lactate import and export, respectively, in MDA-MB-231 cells. Its high selectivity for MCT4 over MCT1 positions VB124 as a promising agent for researching cardiac hypertrophy, heart failure, and metabolic disorders [1].

CSN5i-3 is a novel potent oral and selective CSN5/Jab1 inhibitor that inhibits CSN-catalyzed Cul1 deneddylation with an IC50 value of 5.8 nM.CSN5i-3 exhibits anticancer activity, inhibits cell proliferation and induces apoptosis in human breast cancer cells.

Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity, inhibiting PI3Kβ γ δ with low activity (IC50=250 290 1200 nM). Alpelisib demonstrates antitumor activity and specifically targets PIK3CA mutant tumors.

SIRT1-IN-1, a selective SIRT1 inhibitor with an IC50 of 205 nM, also demonstrates antiviral activity as an inhibitor of cytomegalovirus (CMV).

MF-094 is a potent and selective inhibitor of USP30 with an IC50 of 120 nM.

BOS-318 is a Furin inhibitor with slowly dissociating, highly selective, and cell-pemeable characteristcs.